| pubmed-article:15671650 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15671650 | lifeskim:mentions | umls-concept:C1514743 | lld:lifeskim |
| pubmed-article:15671650 | lifeskim:mentions | umls-concept:C0000854 | lld:lifeskim |
| pubmed-article:15671650 | lifeskim:mentions | umls-concept:C0022009 | lld:lifeskim |
| pubmed-article:15671650 | lifeskim:mentions | umls-concept:C0022023 | lld:lifeskim |
| pubmed-article:15671650 | lifeskim:mentions | umls-concept:C0035930 | lld:lifeskim |
| pubmed-article:15671650 | lifeskim:mentions | umls-concept:C1519941 | lld:lifeskim |
| pubmed-article:15671650 | lifeskim:mentions | umls-concept:C1510438 | lld:lifeskim |
| pubmed-article:15671650 | pubmed:issue | 5 | lld:pubmed |
| pubmed-article:15671650 | pubmed:dateCreated | 2005-1-26 | lld:pubmed |
| pubmed-article:15671650 | pubmed:abstractText | M-channels (M-current), encoded by KCNQ2/3 K(+) channel genes, have emerged as novel drug targets for a number of neurological disorders. The lack of direct high throughput assays combined with the low throughput of conventional electrophysiology (EP) has impeded rapid screening and evaluation of K(+)-channel modulators. Development of a sensitive and efficient assay for the direct measurement of M-current activity is critical for identifying novel M-channel modulators and subsequent investigation of their therapeutic potential. Using a stable CHO cell line expressing rat KCNQ2/3 K(+) channels confirmed by EP, we have developed and validated a nonradioactive rubidium (Rb(+)) efflux assay in a 96-well plate format. The Rb(+) efflux assay directly measures the activity of functional channels by atomic absorption spectroscopy using the automated Ion Channel Reader (ICR) 8000. The stimulated Rb(+) efflux from KCNQ2/3-expressing cells was blocked by the channel blockers XE991 and linopirdine with IC(50) values of 0.15 microM and 1.3 microM, respectively. Twelve compounds identified as KCNQ2/3 openers were further assessed in this assay, and their EC(50) values were compared with those obtained with EP. A higher positive correlation coefficient between these two assays (r = 0.60) was observed than that between FlexStation membrane potential and EP assays (r = 0.23). To simplify the assay and increase the throughput, we demonstrate that EC(50) values obtained by measuring Rb(+) levels in the supernatant are as robust and consistent as those obtained from the ratio of Rb(+) in supernatant/lysate. By measuring the supernatant only, the throughput of ICR8000 in an eight-point titration is estimated to be 40 compounds per day, which is suitable for a secondary confirmation assay. | lld:pubmed |
| pubmed-article:15671650 | pubmed:language | eng | lld:pubmed |
| pubmed-article:15671650 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15671650 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15671650 | pubmed:month | Oct | lld:pubmed |
| pubmed-article:15671650 | pubmed:issn | 1540-658X | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:TengC TCT | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:LuQiangQ | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:KowalDianneD | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:DunlopJohnJ | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:WangKeweiK | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:HeLanL | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:IlesDebraD | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:JowFloraF | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:TsengEugeneE | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:McIlvainBealB | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:ZhangHowardH | lld:pubmed |
| pubmed-article:15671650 | pubmed:author | pubmed-author:ShanQin... | lld:pubmed |
| pubmed-article:15671650 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15671650 | pubmed:volume | 2 | lld:pubmed |
| pubmed-article:15671650 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15671650 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15671650 | pubmed:pagination | 525-34 | lld:pubmed |
| pubmed-article:15671650 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:15671650 | pubmed:meshHeading | pubmed-meshheading:15671650... | lld:pubmed |
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| pubmed-article:15671650 | pubmed:meshHeading | pubmed-meshheading:15671650... | lld:pubmed |
| pubmed-article:15671650 | pubmed:meshHeading | pubmed-meshheading:15671650... | lld:pubmed |
| pubmed-article:15671650 | pubmed:meshHeading | pubmed-meshheading:15671650... | lld:pubmed |
| pubmed-article:15671650 | pubmed:meshHeading | pubmed-meshheading:15671650... | lld:pubmed |
| pubmed-article:15671650 | pubmed:meshHeading | pubmed-meshheading:15671650... | lld:pubmed |
| pubmed-article:15671650 | pubmed:meshHeading | pubmed-meshheading:15671650... | lld:pubmed |
| pubmed-article:15671650 | pubmed:year | 2004 | lld:pubmed |
| pubmed-article:15671650 | pubmed:articleTitle | Validation of an atomic absorption rubidium ion efflux assay for KCNQ/M-channels using the ion Channel Reader 8000. | lld:pubmed |
| pubmed-article:15671650 | pubmed:affiliation | Discovery Neuroscience, Wyeth Research, CN-8000, Princeton, NJ 08543, USA. wangk@wyeth.com | lld:pubmed |
| pubmed-article:15671650 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:15671650 | pubmed:publicationType | Comparative Study | lld:pubmed |
| pubmed-article:15671650 | pubmed:publicationType | Validation Studies | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:15671650 | lld:pubmed |
